1148008-01-8Relevant articles and documents
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach
Barton, Nick,Convery, Máire,Cooper, Anthony W. J.,Down, Kenneth,Hamblin, J. Nicole,Inglis, Graham,Peace, Simon,Rowedder, James,Rowland, Paul,Taylor, Jonathan A.,Wellaway, Natalie
, p. 11061 - 11073 (2019/01/08)
A deconstruction of previously reported phosphoinositide 3-kinase δ (PI3Kδ) inhibitors and subsequent regrowth led to the identification of a privileged fragment for PI3Kδ, which was exploited to deliver a potent, efficient, and selective lead series with a novel binding mode observed in the PI3Kδ crystal structure.